A method for the purification of cyclic indole compounds that provides advantages over previously-known methods. Using the method of the present invention allows for the facile preparation of a good quality solid form of these compounds.

This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R.sub.1:-alkylenyl-C(O)NH-alkylenyl-R.sub.3, -alkylenyl-C(O)O—R.sub.4, R.sub.3:—COOH, —OH, —SH, —NH.sub.2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R.sub.4: H, succinimidyl group, R.sub.2: —H,-alkyl. In II: R.sub.1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R.sub.2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN).sub.2, —HC═CHNO.sub.2, -alkylenyl-NH.sub.2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.

The invention relates to a family of compounds that comprise fluorescent cyanine dyes. The compounds are near infrared absorbing heptamethine cyanine dyes with a 4,4-disubstituted cyclohexyl ring as part of the polymethine chromophore. The compounds are generally hydrophilic and can be chemically linked to biomolecules, such as proteins, nucleic acids, and therapeutic small molecules. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications.

The invention relates to a marking precursor incorporating a chelator or fluorination group for radiolabelling with 44Sc, 47Sc, 55Co, 62Cu, 64Cu, 67Cu, 66Ga, 67Ga, 68Ga, 89Zr, 86Y, 90Y, 90Nb, 99mTc, 111ln, 135Sm, 140Pr, 159Gd, 149Tb, 160Tb, 161Tb, 165Er, 166Dy, 166Ho, 175Yb, 177Lu, 186Re, 188Re, 213Bi and 225Ac or with 18F, 131I or 211At, and one or two biological targeting vectors which are coupled to the chelator or fluorinating group via one or more squaric acid groups.

The invention relates to a family of compounds that comprise fluorescent cyanine dyes. The compounds are near infrared absorbing heptamethine cyanine dyes with a 4,4-disubstituted cyclohexyl ring as part of the polymethine chromophore. The compounds are generally hydrophilic and can be chemically linked to biomolecules, such as proteins, nucleic acids, and therapeutic small molecules. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications.

Systems for use as a medicament for cancers selected from esophagus, pharynx and larynx, lung, brain, and intestines, include a targeting molecule for binding necrotic cells, a chelator, and a radionuclide, to a dosage comprising the system. In particular, the systems relate to compositions targeting necrotic cells.

Provided herein are compounds useful as imaging agents. Exemplary compounds provided herein are useful as myeloperoxidase imaging agents using positron emission tomography or fluorescence imaging techniques. Methods for preparing the compounds provided herein and diagnostic methods using radiolabeled and unlabeled compounds are also provided.

A device for synthesizing a radioisotope-labelled target tracer includes a microfluidic chip having an SCX module configured to concentrate and capture a radioisotope from a radioisotope solution and release the captured radioisotope therefrom, an SAX module configured to purify the released radioisotope from the SCX module, and an passive in-plane mixing/reaction module configured to mix the purified radioisotope with a target precursor and perform labelling reaction to synthesize the radioisotope-labelled target tracer therein. The device also includes a heating means positioned in relation to the microfluidic chip for heating the microfluidic chip during the labelling reaction; and a first valve fluidically coupled with the SCX and SAX modules and a second valve fluidically coupled with the SAX module and the in-plane mixing/reaction module for operably controlling transit of various substances or mixtures among the SCX module, the SAX modules and the in-plane mixing/reaction module.

A method of preparing a .sup.64Cu-BaBaSar-RGD.sub.2 solution is provided. The method includes lyophilizing a solution of BaBaSar-RGD.sub.2 and adding a .sup.64Cu solution to the lyophilized BaBaSar-RGD.sub.2.

Provided is a stable pharmaceutical composition comprising a labeling moiety-anti-human antibody Fab fragment conjugate, and the like. In the pharmaceutical composition comprising a labeling moiety-anti-human antibody Fab fragment conjugate, citric acid, phosphoric acid, 2-[4-(2-hydroxyethyl)-1-piperazinyl]ethanesulfonic acid or trishydroxymethyl aminomethane is added as a buffering agent, sucrose or glycerin is added as a stabilizer, a nonionic surfactant is added, and the pH is adjusted to 6.5 to 7.5. This enables suppression of generation of multimers and insoluble subvisible particles during preservation of the labeling moiety-anti-human antibody Fab fragment conjugate.